A61K38/03

TREATMENT AND PREVENTION OF ALZHEIMER'S DISEASE (AD)

Disclosed is a method for the treatment of AD, wherein an immune stimulating pharmaceutical composition comprising an aluminium salt is administered to a patient having AD or having a risk to develop AD in an effective amount.

Prodrugs comprising an GLP-1/glucagon dual agonist linker hyaluronic acid conjugate

The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an GLP-1/Glucagon agonist linker conjugate Z-L.sup.1-L.sup.2-L-YR.sup.20, wherein Y represents an GLP-1/Glucagon agonist moiety; and -L is a linker moietyby formula (Ia), wherein the dashed line indicates the attachment to one of the amino groups of the GLP-1/Glucagon agonist moiety by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said prodrugs as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by GLP-1/Glucagon agonist. ##STR00001##

PROTEASOME INHIBITORS
20200325171 · 2020-10-15 ·

The present invention relates to a compound of formula (I), wherein X is CO, CS or BOH; Y is an electrophile and Z is a leaving group, or YZ is an electrophile; R.sup.1 comprises or consists of (a) (i) a first group binding to a proteolytic site of a proteasome, said first group being bound to X; and (ii) optionally a second group enhancing delivery; or (b) a group binding between subunits 1 and 2 of a proteasome; R.sup.2 and R.sup.3 are independently selected from H, methyl, methoxy, ethyl, ethenyl, ethinyl and cyano, wherein methyl and ethyl maybe substituted with OH or halogen.

##STR00001##

FORMULATION FOR ORAL DELIVERY OF PROTEINS, PEPTIDES AND SMALL MOLECULES WITH POOR PERMEABILITY

The present disclosure is directed to a pharmaceutical formulation intended for oral delivery of synthetic or natural poorly permeable molecules or salts/solvates thereof having a therapeutic activity. The pharmaceutical formulation can include a synthetic or natural poorly permeable molecule or salt or solvate thereof in an amount 0.01-10 wt. % of the total weight of the formulation; a lipophilic phase comprising triglycerides of fatty acids in an amount of 50-80 wt. % of the total weight of the formulation; and at least one lipophilic surfactant comprising partial esters of polyol and fatty acids in an amount of about 10-50 wt. % of the total weight of the formulation.

FORMULATION FOR ORAL DELIVERY OF PROTEINS, PEPTIDES AND SMALL MOLECULES WITH POOR PERMEABILITY

The present disclosure is directed to a pharmaceutical formulation intended for oral delivery of synthetic or natural poorly permeable molecules or salts/solvates thereof having a therapeutic activity. The pharmaceutical formulation can include a synthetic or natural poorly permeable molecule or salt or solvate thereof in an amount 0.01-10 wt. % of the total weight of the formulation; a lipophilic phase comprising triglycerides of fatty acids in an amount of 50-80 wt. % of the total weight of the formulation; and at least one lipophilic surfactant comprising partial esters of polyol and fatty acids in an amount of about 10-50 wt. % of the total weight of the formulation.

INHIBITORS

The present invention relates to compounds having the formula [Co-enzyme A or analogue thereof]-Z1-Z2-Z3-Z4, wherein Z1 is a linker, Z2 and Z3 are peptides or peptide-based moieties, and Z4 is a C-terminal group. The invention also provides pharmaceutical compositions comprising compounds of the invention, and their uses for the treatment of cancer, wound healing and nerve regeneration, inter alia.

INHIBITORS

The present invention relates to compounds having the formula [Co-enzyme A or analogue thereof]-Z1-Z2-Z3-Z4, wherein Z1 is a linker, Z2 and Z3 are peptides or peptide-based moieties, and Z4 is a C-terminal group. The invention also provides pharmaceutical compositions comprising compounds of the invention, and their uses for the treatment of cancer, wound healing and nerve regeneration, inter alia.

MALIGNANT TUMOR TARGET PEPTIDE

The present invention provides a peptide comprising the amino acid sequence of any of the formulas (I)-(III) below:

(I) an amino acid sequence of (X1) [D] P [D] (X2) [D] wherein X1 is W or F, X2 is S or T, and each amino acid symbol immediately followed by symbol [D] is a D form of the amino acid,
(II) an amino acid sequence of P[D]T[D] (X).sub.n F[D] wherein (X).sub.n is any amino acid in the number of n selected independently of each other, n is an integer of 0-4, and the symbol [D] is as defined above,
(III) an amino acid sequence that is a Retro-inverso of the amino acid sequence of any of the aforementioned (I) and the aforementioned (II);
and a conjugate containing the peptide and a functional part.

MALIGNANT TUMOR TARGET PEPTIDE

The present invention provides a peptide comprising the amino acid sequence of any of the formulas (I)-(III) below:

(I) an amino acid sequence of (X1) [D] P [D] (X2) [D] wherein X1 is W or F, X2 is S or T, and each amino acid symbol immediately followed by symbol [D] is a D form of the amino acid,
(II) an amino acid sequence of P[D]T[D] (X).sub.n F[D] wherein (X).sub.n is any amino acid in the number of n selected independently of each other, n is an integer of 0-4, and the symbol [D] is as defined above,
(III) an amino acid sequence that is a Retro-inverso of the amino acid sequence of any of the aforementioned (I) and the aforementioned (II);
and a conjugate containing the peptide and a functional part.

Methods for the treatment of mitochondrial diseases associated with a mutation in <i>SURF 1 </i>or <i>POLG </i>gene resulting in a disruption of mitochondrial oxidative phosphorylation
10793597 · 2020-10-06 · ·

The disclosure provides methods of preventing, ameliorating or treating disruption of mitochondrial function and symptoms thereof. The methods provide administering aromatic-cationic peptides in effective amounts to prevent, treat or ameliorate the disruption of mitochondrial oxidative phosphorylation in a cell such as that found in a subject suffering from, or predisposed to a mitochondrial disease or disorder. In some embodiments, the methods comprise administering to a subject suffering from, or at risk for a mitochondrial disease or disorder, an effective amount of an aromatic-cationic peptide to subjects in need thereof.